34 results about "Valproic Acid" patented technology

The invention discloses application of Trolox in preparation of a medicine for treating toxicity caused by valproic acid, and belongs to the technical field of biological medicine. The invention discovers for the first time that Trolox has a new medicine application of preventing and / or treating developmental toxicity caused by valproic acid or redox level imbalance caused by valproic acid; furthermore, animal experiments prove that Trolox can relieve zebra fish development malformation caused by valproic acid and also can relieve zebra fish redox level imbalance caused by valproic acid; this provides a new solution for the prevention and / or treatment of developmental toxicity caused by valproic acid or redox level imbalance caused by valproic acid.

The present invention relates to a pharmaceutical composition for oral administration, the pharmaceutical composition comprising: a) immediate-release granules comprising i. an active ingredient selected from the group consisting of valproic acid, semi-sodium valproic acid, sodium valproic acid, and magnesium valproic acid, and ii. a filler; and b) sustained-release pellets comprising: i. a pellet core comprising (1) an active ingredient selected from the group consisting of valproic acid, semi-sodium valproic acid, sodium valproic acid, and magnesium valproic acid, and (2) a filler; and ii. on the pellet core iii. A sustained-release pellet comprising a subcoat provided on the subcoat, the content of which is 10 to 20% by weight based on the weight of the pellet core and contains a film-forming agent, and iii. a sustained-release coating provided on the subcoat, the content of which is 25 to 100% by weight based on the weight of the pellet core coated with the subcoat and contains a film-forming agent, wherein the amount of active ingredient in the immediate-release granules accounts for 70 to 80% by weight of the total weight of active ingredients in the pharmaceutical composition, and the amount of active ingredient in the sustained-release pellets accounts for 20 to 30% by weight of the total weight of active ingredients in the pharmaceutical composition. In yet another aspect, the present invention relates to a method for producing a pharmaceutical composition and a pharmaceutical composition for use in a method of pretreatment of cancer.

The present invention relates to methods of treating / preventing abnormal conditions associated with pulmonary arterial hypertension (PAH) and methods of treating PAH in subjects refractory to treatment for PAH, said methods involving administering to the subject of an effective amount of a of Formula (I), wherein R1 is either H or D and wherein D is deuterium, or a pharmaceutically acceptable salt thereof.

This invention relates to the field of biomedical technology, specifically disclosing the application of betaine in the preparation of drugs for treating autism. Through experiments using a valproic acid-induced mouse model of autism spectrum disorder, this invention found that betaine can significantly improve social impairments and repetitive, stereotyped behaviors in the model mice, and exhibits stable and reproducible effects in both 1-month-old and 2-month-old male offspring. This invention reveals a novel use of betaine in treating core behavioral deficits in autism spectrum disorder (ASD), providing a new source of natural active ingredients for the preparation of drugs for treating autism.

The present technology generally relates to methods of treating social deficits with HDAC inhibitors. Select embodiments of the present technology include a method for treating organophosphate induced social deficits in a subject, comprising administering to a subject in need thereof a therapeutically effective amount of an HDAC inhibitor selected from the group consisting of valproic acid, butyric acid, BRD-6929, RGFP966, pharmaceutically acceptable salts thereof, and combinations thereof. The subject may have been diagnosed with a disease or disorder characterized by social deficits, such as autism spectrum disorder. The subject may be monitored for a change in the severity of social deficits.

The present invention relates to a combination of valproic acid (VPA) and S- adenosylmethionine (SAMe) for use in preventing congenital malformations in a fetus of a subject in need of VPA treatment and who is pregnant or intends to become pregnant, by administering the combination to the subject before or during the first trimester of pregnancy, wherein the SAMe and the VPA are at a ratio of about 1:10-1:50 w / w SAMe:VPA in the combination; and corresponding methods of treatment.

The present application relates to the technical field of pharmaceutical chemistry, and particularly relates to lithium valproate and crystal forms thereof, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. The crystal forms of lithium valproate comprise crystal form I, crystal form II, crystal form III, crystal form IV, crystal form V, crystal form VI and crystal form VII.

The application discloses a kind of HPLC-MSMS method for simultaneously determining valproic acid, olanzapine and its metabolites in plasma, which comprises the following steps: S1. pretreatment of plasma samples with acetonitrile protein precipitation method;S2. HPLC-MSMS method is used to detect plasma samples, and qualitative and / or quantitative analysis of valproic acid, olanzapine and its metabolites in plasma is carried out simultaneously;Wherein, Agilent Poroshell 120EC-C18 column is selected as the chromatographic column;Electrospray ion source is used, and the mobile phase is A phase: formic acid water, B phase: acetonitrile;By optimizing the conditions of liquid phase and mass spectrometry, valproic acid, olanzapine and its metabolites are simultaneously determined by one method.The method has been applied to detect plasma samples of olanzapine and valproic acid combination, and olanzapine alone, and the measured results all meet the linear range.

The present invention relates to valproic acid for use in treating and / or preventing pulmonary arterial hypertension (PAH), wherein the treatment and / or prevention comprises administering to a subject a total daily dose of from about 200 mg to about 600 mg of valproic acid or a pharmaceutically acceptable salt thereof.

The invention discloses application of valproic acid in preparation of a medicine for resisting jewfish iridovirus. 24 mM of VPA is non-toxic to LJFin, and the effective use concentration of VPA for inhibiting SPIV infection in in-vitro cells is 3-24 mM. Through three administration modes of pretreatment, co-treatment and post-treatment, the VPA has the effects of preventing and treating SPIV infection. The VPA plays a role in resisting SPIV infection mainly by inhibiting entry and release of viruses, and has no obvious influence on adsorption of the viruses. In addition, after being fed as a feed additive, the feed additive does not affect ingestion and fish body health, and shows a good ability of enhancing the SPIV resistance of jewfish. According to the present invention, the death rate caused by SPIV infection is reduced by adding 0.25% and 0.5% of the VPA to the feed, the relative protection rates on SPIV are 21.1% and 31.6%, the virus replication in the tissue can be inhibited, and the virus-induced fish target tissue structure damage can be reduced; as an antiviral drug, VPA has a certain application value in prevention and control of jewfish iridovirus diseases.

The present disclosure relates to a combination of valproic acid or a pharmaceutically acceptable salt thereof, a β-lactam compound or a pharmaceutically acceptable salt thereof, and probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing disease using this combination.

This application relates to the field of analytical detection technology, specifically to sample pretreatment methods, kits, and detection methods for the detection of antiepileptic drugs. The sample pretreatment method for the detection of antiepileptic drugs in this application includes one or more of the following antiepileptic drugs: valproic acid, carbamazepine, phenytoin, levetiracetam, lamotrigine, and phenobarbital. The sample pretreatment method includes the following steps: mixing magnetic beads with an activation solution to prepare a magnetic bead suspension; mixing the sample to be tested, the magnetic bead suspension, and an internal standard solution, and separating the supernatant and the magnetic bead complex after magnetic adsorption treatment; adding an eluent to the magnetic bead complex, and collecting the magnetic bead-target complex after elution treatment; adding an elution buffer to the magnetic bead-target complex, and collecting the supernatant after elution treatment for detection. The above sample pretreatment method is simple to operate, time-saving, and low-cost, providing key technical support for the efficient quantitative detection of antiepileptic drugs.

The invention relates to the field of biological medicine, in particular to a three-component platinum (IV) complex containing captopril (CTP) and valproic acid (VPA), a preparation method of the three-component platinum (IV) complex and application of the three-component platinum (IV) complex in preparation of anti-tumor proliferation and anti-metastasis drugs. The anti-tumor proliferation and anti-metastasis effects of the target compound are tested through in-vivo and in-vitro testing means, and the anti-tumor mechanism of the medicine is researched. Results prove that the compound has a remarkable anti-tumor capability, particularly has an excellent treatment effect on metastatic malignant tumors, is expected to provide a new candidate drug for clinical treatment of tumors, and provides a new direction for research and development of novel platinum drugs and anti-tumor metastasis drugs.

The invention relates to a pharmaceutical composition for oral administration. The pharmaceutical composition comprises: a) immediate release particles comprising i. An active ingredient selected from the group consisting of valproic acid, semi-sodium valproate, sodium valproate and magnesium valproate, and ii. A filler, b) sustained release pellets comprising: i. A pellet core comprising (1) an active ingredient selected from the group consisting of valproic acid, semi-sodium valproate, sodium valproate and magnesium valproate, and (2) a filler, ii. A sub-coating disposed on the pellet core, the content of the sub-coating layer is 10-20 wt% based on the weight of the pellet core and the sub-coating layer comprises a film-forming agent, and iii. A slow-release coating layer disposed on the sub-coating layer, the content of the slow-release coating layer is 25-100 wt% based on the weight of the pellet core coated with the sub-coating layer and the slow-release coating layer comprises a film-forming agent, and the content of the slow-release coating layer is 25-100 wt% based on the weight of the pellet core coated with the sub-coating layer. Wherein the amount of the active ingredients in the quick-release particles accounts for 70-80 wt% of the total weight of the active ingredients in the pharmaceutical composition, and the amount of the active ingredients in the slow-release pellets accounts for 20-30 wt% of the total weight of the active ingredients in the pharmaceutical composition. In further aspects, the present invention relates to methods of preparing pharmaceutical compositions and pharmaceutical compositions for use in methods of pre-treating cancer.

The application discloses a valproic acid detection kit. Specifically, the application relates to a valproic acid derivative and a preparation method thereof, and a kit containing the valproic acid derivative and a preparation method thereof. The technical scheme of the application uses a novel valproic acid derivative and a coupling method of maleimide-sulfhydryl with high selectivity, so that the derivative and an enzyme are coupled in a 1:1 mode, and batch difference formed in a conventional coupling process is greatly reduced. The valproic acid detection kit is simple, fast and low in cost, and can be automatically detected on various mainstream machines.

The invention provides a composition for reversing organ fibrosis and application of the composition, and belongs to the technical field of biological medicines.The cocktail composition is prepared from valproic acid, CHIR99021, Repsox, trans-benzene ring propylamine and forskolin. The HAT inhibition composition is prepared from A485 and WM-8014; the cocktail composition and the HAT inhibition composition are used independently or jointly, and hepatic fibrosis or pulmonary fibrosis can be reversed; when the composition is used in combination, a synergistic enhancement effect is shown in pulmonary fibrosis and hepatic fibrosis models, and the effects of improving fibrosis indexes and reversing epigenetic age are more remarkable; according to the composition provided by the invention, the epigenetic procedure of cells is accurately controlled, so that the cells are safely reversed from a pathological state to a healthy or resting state, the pathological phenotype of fibrosis is improved, the biological age of the cells is fundamentally reversed, and a major breakthrough in the field of fibrosis treatment is represented.

A method of intranasal drug delivery including administering a multi-compartment nanoemulsion to a nasal cavity of a subject in need thereof, where the multi-compartment nanoemulsion includes a water-in-oil core emulsion having an oil phase encompassing a first aqueous phase, the oil phase comprising a first surfactant and a fatty acid and the first aqueous phase comprising levetiracetam and valproic acid dissolved therein. The multi-compartment nanoemulsion further includes a second aqueous phase encompassing the water-in-oil core emulsion, the second aqueous phase comprising a second surfactant and a co-surfactant in a ratio of the second surfactant to the co-surfactant of 1:4 to 4:1. The multi-compartment nanoemulsion has an average droplet size of less than 100 nm and a polydispersity index (PDI) of 0.1 to 0.2.

The invention relates to the technical field of analysis and detection, in particular to a sample pretreatment method for anti-epileptic drug detection, a kit and a detection method. According to the sample pretreatment method for anti-epileptic drug detection, an anti-epileptic drug comprises one or more of valproic acid, carbamazepine, phenytoin, levetiracetam, lamotrigine and phenobarbital; the sample pretreatment method comprises the following steps: mixing magnetic beads with an activating solution to prepare a magnetic bead suspension; mixing a to-be-detected sample, the magnetic bead suspension and the internal standard solution, performing magnetic attraction treatment, and separating supernate and a magnetic bead compound; leacheate is added into the magnetic bead compound, and after leaching treatment, a magnetic bead-target compound is collected; and adding an eluent into the magnetic bead-target compound, carrying out elution treatment, and collecting a supernatant for detection. The sample pretreatment method is simple to operate, short in time consumption and low in cost, and can provide key technical support for efficient quantitative detection of the anti-epileptic drugs.

A stable pharmaceutical composition in the form of orally administrable prolonged release tablet comprising sodium valproate and valprioic acid with no granulating solvent is disclosed, further comprising low viscosity polymer, high viscosity polymer, binder, adsorbent and glidant. A process for the preparation of said orally administrable prolonged release tablet is also disclosed.

The invention relates to a method for treating cancers. Many cancers harbour sternness signature to de-differentiate into immature progenitors confer to tumor clones the re-expression of genes from fetal development. Inventors have obtained mice per group which received two boosts of vaccine 7 and 14 days with 2×106 irradiated hESCs cells that were mixed with 3 different adjuvants: 500 μg of TLR3, 50 μg of TLR9 agonist or 50 μg / ml of Quil A® Saponin vaccine adjuvant. After 14 days 5×104 4T1 cells were injected into the mammary fat pad of the mice and Valproic acid added in the drinking water at the dose of 4 mg / ml. They have shown that in contrast to the non-vaccinated mice, the mice vaccinated with hESC combined with a TLR3 agonist have generated the highest reduction of breast tumor volume (p<0.001) compared to the use of a TLR9 agonist or to Quil-A® Saponin vaccine adjuvant. Accordingly, the invention relates to a method for treating a subject suffering from a cancer with i) an agent that induces MHC-I presentation of antigens, ii) a vaccine composition containing an immunogenic element and iii) an adjuvant.

The invention relates to a method for detecting impurities in a process for preparing valproic acid, sodium valproate or magnesium valproate by atom economy reaction, which comprises the following steps of: selecting a gas chromatograph with the model of Agilent 8890, and detecting valproic acid prepared by atom economy reaction and process impurities thereof by gas chromatography; the detection conditions of the gas chromatography are as follows: a chromatographic column is DB-FFAP, and the specification is 0.32 mm * 60 m, 0.5 [mu] m; the carrier gas is nitrogen; the detector is an FID (Flame Ionization Detector); the flow rate is 2ml / min; the sample injection volume is 2 microliters; the temperature of a sample inlet is 220 DEG C; the column temperature is 100 DEG C; in the heating procedure, the initial temperature is 100 DEG C and kept for 5 min, then the temperature is increased to 140 DEG C at the speed of 4 DEG C / min and kept for 5 min, and then the temperature is increased to 200 DEG C at the speed of 4 DEG C / min and kept for 15 min; the operation time is 50 min; the temperature of a detector is 220 DEG C; the method comprises the following steps of: injecting 2 microliters of diluent dichloromethane, 2 microliters of reference solution and 2 microliters of test solution into a gas chromatograph, and recording a chromatogram; a test article is selected from a valproic acid crude product prepared by atom economy reaction; the impurities are selected from 2-propyl-4-pentenoic acid, valeric acid, 2-methyl valeric acid, 2-ethyl valeric acid, methyl valproate, ethyl valproate or propyl valproate; the solvent is a solvent; according to the detection result of the gas chromatography, the variety and the content of the process impurities in the valproic acid, the sodium valproate or the magnesium valproate are judged through a control sample.

A compound of formula (I) is disclosed: [Refer to original abstract doc for image] where R1 is either H or D, and D is deuterium; or valproic acid, or a pharmaceutically acceptable salt thereof, for u

Valproic acid, or a compound of Formula (I), or a pharmaceutically acceptable salt thereof: [Refer to original abstract doc for image] wherein R1 is H or D and D is deuterium, for use in the treatment

This invention relates to the use of valproic acid in constructing animal models of dilated cardiomyopathy, and to a method for constructing such an animal model and screening drugs, belonging to the field of pharmaceutical technology. This invention involves administering 50-100 μM valproic acid to zebrafish farms. The dilated cardiomyopathy animal model constructed by this invention complements existing models. In drug screening applications, this complementarity effectively avoids the missed screening of candidate active compounds due to the limitations of a single model mechanism, significantly improving the comprehensiveness and success rate of screening. Simultaneously, the phenotype of the drug screening model of this invention is highly consistent with clinical findings, the model construction cycle is short and low-cost, and it can achieve dynamic visualization and be applied to high-throughput drug screening.

The invention provides a culture medium for inducing secretion of stem cell factors and application of the culture medium, and belongs to the technical field of cell biology. The culture medium adopts a three-stage dynamic induction strategy and comprises a starting culture medium (containing CHIR99021 and valproic acid), an induction culture medium (containing Forskolin, SR3677 and melatonin) and a maintenance amplification culture medium (containing ISX-9 and resveratrol). Through staged and accurate small molecule stimulation, the paracrine function of the cord blood mesenchymal stem cells can be efficiently and synergistically enhanced, and the secretion level of multiple therapeutic factors such as SCF, VEGF, HGF and IGF-1 is remarkably improved. Therefore, the invention provides a safe and stable culture system with definite components, the culture system is used for obtaining a high-activity stem cell secretion product, and the product can be applied to preparation of an external gel preparation for promoting skin wound healing and has important clinical transformation value.

The invention relates to application of an AQP7 inhibitor in preparation of a medicine for preventing and treating ATO cardiotoxicity, and belongs to the technical field of medicines. In order to relieve ATO cardiotoxicity, the invention provides application of an AQP7 inhibitor in preparation of drugs for preventing and treating ATO cardiotoxicity, and the AQP7 inhibitor is siRNA or valproic acid. The invention proves that the accumulation of ATO in heart tissues is a key factor for inducing cardiotoxicity for the first time, and targeted inhibition of AQP7 can significantly reduce the accumulation level of ATO in the heart and alleviate myocardial structure damage and inflammatory infiltration caused by ATO. The invention finds that valproic acid can be used as an efficient inhibitor of AQP7 for the first time, specifically inhibits AQP7, reduces accumulation of ATO in heart, and effectively relieves cardiotoxicity. By inhibiting the AQP7, the cardiac toxicity of the ATO can be remarkably reduced on the premise of not influencing the anti-tumor curative effect of the ATO.

This invention discloses a valproic acid chemiluminescent immunoassay reagent and its preparation and detection methods. The immunoassay reagent, developed using a high-titer anti-valproic acid specific antibody, can accurately determine the valproic acid content in serum and plasma samples. Compared with traditional methods, the valproic acid chemiluminescent immunoassay reagent provided by this invention has high sensitivity and specificity. When used in conjunction with a chemiluminescent immunoassay analyzer, it offers advantages such as ease of operation, high throughput, and accurate detection results, which is of great significance for guiding rational drug use in clinical practice.

The invention discloses olfactory mucosa mesenchymal stem cells with efficient differentiation potential and a preparation method of the olfactory mucosa mesenchymal stem cells, and relates to the technical field of cell culture. According to the method, firstly, a complete culture medium special for the olfactory mucosa mesenchymal stem cells is prepared, after chondroitin sulfate, valproic acid, a fibroblast growth factor (FGF) and a nerve growth factor (NGF) are added into the culture medium, the in-vitro proliferation speed of the human olfactory mucosa mesenchymal stem cells is greatly increased by promoting expression of syndecan 1, and the survival rate of the human olfactory mucosa mesenchymal stem cells is increased; meanwhile, it is guaranteed that the stem cells still maintain an undifferentiated state after multi-generation proliferation, and the stem cells have high stem cell property. The olfactory mucosa mesenchymal stem cells pretreated by using the culture medium have stronger capability of differentiating to neurons, and can be better applied to diseases related to neural restoration.

The invention discloses a valproic acid loaded ZIF-8 nano composite material as well as a preparation method and application thereof, and belongs to the cross technical field of biomedical materials and oral medicine. The preparation method of the valproic acid loaded ZIF-8 nano composite material comprises the following steps: dispersing ZIF-8 nano particles in a solvent, and adding valproic acid into the solvent to load the valproic acid, so as to obtain the valproic acid loaded ZIF-8 nano composite material. The VPA-ZIF8 nano composite material provided by the invention integrates multiple functions of resisting bacteria, resisting inflammation and promoting regeneration, the treatment effect on dental pulp injury is remarkably improved, the defects in the prior art are overcome, and the VPA-ZIF8 nano composite material has important innovativeness and practical value.